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METHODS AND INTERMEDIATES FOR THE PREPARATION OF (4BS,5AR)-12-CYCLOHEXYL-N-(N,N-DIMETHYLSULFAMOYL)-3- METHOXY-5A-((1R,5S)-3-METHYL-3,8-DIAZABICYCLO3.2.1OCTANE-8-CARBONYL)-4B,5,5A,6-TETRAHYDROBENZO 3,4CYCLOPROPA5,6AZEPINO1,2-AINDOLE-9-CARBOXAMIDE

机译：制备（4BS，5AR）-12-环己基-N-（N，N-二甲基巯基磺酰基）-3-甲氧基-5A-（（（1R，5S）-3-甲基-3,8-DIAZABICYCLO [的方法和中间体] 3.2.1] OCTANE-8-CARBONYL）-4B，5,5A，6-TEHYDROBENZO [3,4] CYCLOPROPA [5,6] AZEPINO [1,2-A] INDOLE-9-CARBOXAMIDE

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摘要

The present invention provides methods and intermediates for the preparation of (1aR, 12bS)-8-cyclohexyl-11-fluoro-N-((1-methylcyclopropyl)sulfonyl)-1a-((3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl)carbonyl)-1,1a,2,12b-tetrahydrocyclopropa[d]indolo[2,1-a][2]benzazepine-5-carboxamide (formula I), including pharmaceutically acceptable salts. The compound has activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

机译：本发明提供了用于制备（1a R ，12b S ）-8-环己基-11-氟- N -的方法和中间体。（（1-甲基环丙基）磺酰基）-1a-（（3-甲基-3,8-二氮杂双环[3.2.1] oct-8-基）羰基）-1,1a，2,12b-四氢环丙烷[d] ] indolo [2,1- a ] [2] benzazepine-5-carboxamide（式I），包括可药用的盐。该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗被HCV感染的人。 <图像文件=“ IMGA0001.GIF” he =“ 55” imgContent =“ chem” imgFormat =“ GIF” wi =“ 69” /> 展开▼

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公开/公告号EP3091022A3

专利类型

公开/公告日2016-12-14

原文格式PDF

申请/专利权人 BRISTOL-MYERS SQUIBB HOLDINGS IRELAND;
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申请/专利号EP20160172744

发明设计人 DELMONTE ALBERT J.;NATALIE JR. KENNETH J.;FRAUNHOFFER KENNETH J.;RISATTI CHRISTINA ANN;HANG CHAO;GAO ZHINONG;DAVULCU AKIN H.;HU WENHAO;
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申请日2013-07-16

分类号C07D519;C07D487/04;A61K31/55;A61P31/14;

国家 EP

入库时间 2022-08-21 14:03:29

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专利

1. 用于制备(4bS,5aR)-12-环己基-N-(N,N-二甲基氨磺酰基)-3-甲氧基-5a-((1R,5S)-3-甲基-3,8-二氮杂二环3.2.1辛烷-8-羰基)-4b,5,5a,6-四氢苯并3,4环丙并5,6氮杂并1,2-a吲哚-9-甲酰胺的新颖方法和中间体 [P] . 中国专利： CN104640870A . 2015-05-20

2. (1R,2S,5S)-N-[(1S)-3-氨基-1-(环丁基甲基)-2,3-二氧代丙基]-3-[(2S)-2-[[[(1,1-二甲基乙基)氨基]-羰基]氨基]-3,3-二甲基-1-氧代丁基]-6,6-二甲基-3-氮杂双环[3.1.0]己烷-2-碳酰胺的制备方法 [P] . 中国专利： CN101611000B . 2013.08.21

3. METHODS AND INTERMEDIATES FOR THE PREPARATION OF (4BS,5AR)-12-CYCLOHEXYL-N-(N,N-DIMETHYLSULFAMOYL)-3- METHOXY-5A-((1R,5S)-3-METHYL-3,8-DIAZABICYCLO3.2.1OCTANE-8-CARBONYL)-4B,5,5A,6-TETRAHYDROBENZO 3,4CYCLOPROPA5,6AZEPINO1,2-AINDOLE-9-CARBOXAMIDE [P] . 欧洲知识产权局专利： EP2875030B1 . 2016-10-26

机译：制备（4BS，5AR）-12-环己基-N-（N，N-二甲基巯基磺酰基）-3-甲氧基-5A-（（（R，5S）-3-甲基-3,8-二氮杂双环[ 3.2.1] OCTANE-8-CARBONYL）-4B，5,5A，6-TEHYDROBENZO [3,4] CYCLOPROPA [5,6] AZEPINO [1,2-A] INDOLE-9-CARBOXAMIDE

4. METHODS AND INTERMEDIATES FOR THE PREPARATION OF (4BS,5AR)-12-CYCLOHEXYL-N-(N,N-DIMETHYLSULFAMOYL)-3- METHOXY-5A-((1R,5S)-3-METHYL-3,8-DIAZABICYCLO3.2.1OCTANE-8-CARBONYL)-4B,5,5A,6-TETRAHYDROBENZO 3,4CYCLOPROPA5,6AZEPINO1,2-AINDOLE-9-CARBOXAMIDE [P] . 欧洲知识产权局专利： EP3091022A2 . 2016-11-09

机译：制备（4BS，5AR）-12-环己基-N-（N，N-二甲基巯基磺酰基）-3-甲氧基-5A-（（（1R，5S）-3-甲基-3,8-DIAZABICYCLO [的方法和中间体] 3.2.1] OCTANE-8-CARBONYL）-4B，5,5A，6-TEHYDROBENZO [3,4] CYCLOPROPA [5,6] AZEPINO [1,2-A] INDOLE-9-CARBOXAMIDE

5. NOVEL METHODS AND INTERMEDIATES FOR THE PREPARATION OF (4BS,5AR)-12-CYCLOHEXYL-N-(N,N-DIMETHYLSULFAMOYL)-3-METHOXY-5A-((1R,5S)-3-METHYL-3,8-DIAZABICYCLO3.2.1OCTANE-8-CARBONYL)-4B,5,5A,6-TETRAHYDROBENZO 3,4CYCLOPROPA5,6AZEPINO1,2-AINDOLE-9-CARBOXAMIDE [P] . 韩国专利： KR20150038122A . 2015-04-08

机译：（4BS，5AR）-12-环己基-N-（N，N-二甲基磺酰胺基）-3-甲氧基-5A-（（（1R，5S）-3-甲基-3,8-二氮杂双环）的制备方法和中间体[3.2.1] OCTANE-8-CARBONYL）-4B，5,5A，6-TETRAHYDROBENZO [3,4] CYCLOPROPA [5,6] AZEPINO [1,2-A] INDOLE-9-CARBOXAMIDE